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Design purposes
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Determining key compound properties by experimental assays

The most important things that pharmaceutical companies need to know about new compounds include their solubility, lipophilicity, plasma proten binding and how they are metabolized by the liver. For orally-administered compounds, drug researchers need a measure of gastro-intestinal permeability. Cyprotex can provide a quality-assured technology platform for the evaluation of all of these properties.

As compounds advance through the drug development process their numbers decrease and the level of detail and accuracy needed in evaluating relevant pharmacokinetic properties becomes necessarily greater. Therefore, different methods for pharmacokinetic assessment are employed depending on the stage the compound has reached in the drug development process. Cyprotex has developed a range of assays from high capacity in vitro ADME screening analyses for early discovery projects through to the hand-crafted methods which are necessary at the preclinical stages.

Cloe® Screen microsomal stability - evaluating thousands of compounds reliably and cost-effectively

This assay gives an indication of a compound's potential to be metabolized by the liver and hence whether it will reside in the body long enough to have a sufficient therapeutic effect. It can be easily adapted to investigate potential adverse drug response resulting from drug-drug interactions. The assay measures how quickly the compound disappears when placed in an environment that mimics the model species liver. At Cyprotex, we follow the disappearance of the test substance with liver microsomes - subcellular fractions from liver cells that contain the major liver enzymes involved in compound clearance or by using complete hepatocytes for more accurate, hand-crafted evaluation for a handful of compounds. We are able to generate intrinsic clearance results for both human and rat.


New assay:
Cloe® Select: P-gp inhibition assay
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